NN9056
NN9056 is a selective CCK-1 receptor agonist. NN9056 has an IC50 value of 0.105 nM for the human target and an IC50 value of 0.123 nM for the porcine target. NN9056 inhibits food intake and induces body weight loss. NN9056 improves insulin (Insulin (human)) (HY-P0035) sensitivity secondary to body weight reduction. NN9056 is a long-acting analog with an extended plasma half-life that provides all-day plasma exposure coverage. NN9056 can be used for obesity research.
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- CAS No.: 2064085-67-0
- Formule: C89H133N13O27S
- Masse moléculaire:1849.14
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COS-7 | EC50 |
0.205 nM
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Activation of overexpressed pig CCK-1 receptors in COS-7 cells assessed by IP-One HTRF assay measuring IP1 accumulation.
Activation of overexpressed pig CCK-1 receptors in COS-7 cells assessed by IP-One HTRF assay measuring IP1 accumulation.
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31175319 |
| COS-7 | EC50 |
0.093 nM
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Activation of overexpressed human CCK-1 receptors in COS-7 cells assessed by IP-One HTRF assay measuring IP1 accumulation.
Activation of overexpressed human CCK-1 receptors in COS-7 cells assessed by IP-One HTRF assay measuring IP1 accumulation.
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31175319 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | Tmax | Cmax | AUC | T1/2 |
|---|---|---|---|---|---|---|
| Pig[1] | 5 nmol/Kg | s.c. | 3.4 h | 76.775 nM | 3091 kg·h/L | 128 h |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Landrace × Yorkshire × Duroc (LYD) (female, approximately 3 months old, 30-35 kg)[1]
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Dosage:10 nmol/kg and 100 nmol/kg
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Administration:s.c.; single dose
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Result:Food intake was 86% of vehicle from 0-24 h (corresponding to -1.1 kg) and 75% of vehicle from 25-48 h (corresponding to -0.8 kg).
At 10 nmol/kg, food intake was not significantly reduced and was 22% lower than vehicle from 0-24 h (corresponding to -0.3 kg) and 33% lower from 25-48 h (corresponding to -0.4 kg).
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Animal Model:Landrace × Yorkshire × Duroc (LYD) (female, approximately 3 months old, 30-35 kg)[1]
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Dosage:10 nmol/kg; 20 nmol/kg; 40 nmol/kg; 80 nmol/kg
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Administration:s.c.; single dose
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Result:Food intake was dose-dependently reduced after a single s.c. dose of 10, 20, 40, or 80 nmol/kg.
At 20 and 40 nmol/kg, food intake was significantly reduced for 2 days, and at 80 nmol/kg, food intake was significantly reduced for at least 4 days.
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Animal Model:Göttingen Minipig (female, ovariectomised, approximately 18 months old at study start)[1]
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Dosage:low dose: initially 5 nmol/kg, then 3 nmol/kg, then 2 nmol/kg; high dose: 10 nmol/kg
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Administration:s.c.; once daily; 13 weeks; 3-week wash-out
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Result:Accumulated food intake from days 1-77 was 51.5 kg in the low-dose group and 41.8 kg in the high-dose group.
Body weight change from days 1-77 was -2.3% in the low-dose group and -7.2% in the high-dose group.
During IVGTT, glucose clearance (K_G) was 4.1 min-1 in the low-dose group and 3.4 min-1 in the high-dose group; AUC_insulin was 48.9 nM·min in the low-dose group and 52.0 nM·min in the high-dose group.
Fasting plasma parameters were: low dose-glucose 4.0 mM, insulin 78 pM, C-peptide 24 pM, glucagon 13.5 pM, total GLP-1 37.1 pM, TBA 7.8 µM, TG 0.56 mM, TC 2.1 mM, leptin 38.6 ng/mL HE, α-amylase 1568 U/L, lipase 12.5 U/L; high dose-glucose 4.0 mM, insulin 68 pM, C-peptide 24 pM, glucagon 11.6 pM, total GLP-1 37.6 pM, TBA 9.0 µM, TG 0.41 mM, TC 2.1 mM, leptin 47.2 ng/mL HE, α-amylase 1755 U/L, lipase 9.4 U/L.
Chemical Information
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CAS No. 2064085-67-0
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Masse moléculaire 1849.14
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Formule C89H133N13O27S
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SMILES
NC([C@H](CC1=CC=CC=C1)N(C)C([C@@H](CC(O)=O)N(C)C([C@H](CCCC)NC([C@@H](NC(CNC([C@H](CCCC)NC([C@@H](NC([C@H](CC(O)=O)NC(COCCOCCNC(COCCOCCNC(CC[C@H](NC(CCCCCCCCCCCCCCCCC(O)=O)=O)C(O)=O)=O)=O)=O)=O)CC2=CC=C(C=C2)CS(=O)(O)=O)=O)=O)=O)CC3=CNC4=CC=CC=C34)=O)=O)=O)=O
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Sequence
Asp(AEEA-AEEA-γGlu-C18 diacid)-Phe(4-sulfomethyl)-Nle-Gly-Trp-Nle-DAsp(NMe)-Phe-NH2
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Sequence Shortening
Asp(AEEA-AEEA-γGlu-C18 diacid)-Phe(4-sulfomethyl)-Nle-GW-Nle-DAsp(NMe)-F-NH2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NN9056 Related Classifications
HY-P12402 Related Classifications
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